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http://dx.doi.org/10.7841/ksbbj.2016.31.4.219

Development and Evaluation of Gastro Retentive Floating Matrix Tablet Containing Valsartan Solid Dispersion  

Cho, Young Ho (Department of Pharmaceutics & Biotechnology, Konyang University)
Lee, Jong-Hwa (Division of Research and Development, Korea Institute of Toxicology)
Lee, Gye Won (Department of Pharmaceutics & Biotechnology, Konyang University)
Publication Information
KSBB Journal / v.31, no.4, 2016 , pp. 219-227 More about this Journal
Abstract
Valsartan, a drug for the treatment of cardiovascular disease, exhibited low bioavailability which was caused by, at least in part, limited solubility at low pH. Present investigation deals with the preparation and characterization of gastro-retentive drug delivery system (GRDDS) using valsartan solid dispersion. We prepared solid dispersion using surfactants (Poloxamer 407) and alkalizer ($Na_2CO_3$) which may to be useful for improving solubility of valsartan at low pH and evaluated by saturated solubility of valsartan in distilled water. Valsartan gastro-retentive (GR) tablets containing solid dispersion prepared and evaluated by weight variation, floating time and dissolution rate. Compression at lower pressures resulted in the tablets floating over simulated gastric fluid (pH 1.2) for more than 17 h. In vitro release of valsartan from GR tablet was dependent on the amount of poloxamer 407 and hydroxypropyl methylcellulose. On the basis of evaluation parameter, formulation E-3 was selected as a final formulation. Therefore, it can be concluded that the GR tablets containing solid dispersion may be exploited successfully for the delivery of poorly drug such as valsartan.
Keywords
Valsartan; Gastro-retentive drug delivery system; Solid dispersion; Alkalizer; Hydroxypropyl methylcellulose;
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  • Reference
1 Arora, S., J. Ali, A. Ahuja, R. K. Khar, and S. Baboota (2005) Floating drug delivery systems: A review. AAPS Pharm. Sci. Tech. 6: 372-390.   DOI
2 Kadivar, A., B. Kamlidehghan, H. A. Javar, E. T. Davoudi, N. D. Zaharuddin, B. Sabeti, L. Y. Chung, and M. I. Noordin (2015) Formulation and in vitro, in vivo evaluation of effervescent floating sustained release imatinib mesylate tablet. PLOS One. 10: e0126874.   DOI
3 Kumar, N., S. Soni, T. Singh, A. Kumar, F. J. Ahmad, A. Bhatnagar, and G. Mittal (2015) Development and optimization of gastroretentive controlled-release tablet of calcium-disodium edetate and its in vivo gamma scintigraphic evaluation. AAPS Pharm. Sci. Tech. 16: 1270-1280.   DOI
4 Patel, D. M., M. J. Patel, A. N. Patel, and C. N. Patel (2011) Formulation and evaluation of mixed matrix gastro-retentive drug delivery for famotidine. Int. J. Pharm. Investig. 1: 247-254.   DOI
5 Sharma, N., N. Jain, S. CK, and S. Jain (2012) Formulation and evaluation of gastric retensive floating tablets containing Cefpodoxime proxetil solid dispersions. Int. J. Curr. Pharm. Res. 4: 82-87.
6 Bechgaard, H. and K. Ladefoged (1978) Distribution of pellets in the gastrointestinal tract. The influence on transit time exerted by the density or diameter of pellets. J. Pharm. Pharmacol. 30: 690-692.   DOI
7 Vervaet C., L. Baert, and J. P. Remon (1995) Extrusion-spheronization: A literature review. Int. J. Pharm. 116: 131-146.   DOI
8 Shep, S., S. Dodiya, S. Lahoti, and R. Mayee (2011) Swelling system: a novel approach towards gastroretentive drug delivery system. Indo-Global J. Pharm. Sci. 1: 234-242.
9 Mamajek, R. C. and E. S. Moyer (1980) Drug-dispensing device and method. US Patent 4,207,890.
10 Urquhart, J. and F. Theeuwes (1984) Drug delivery system comprising a reservoir containing a plurality of tiny pills. US Patent 4,434,153.
11 Singh, B. N. and K. H. Kim (2000) Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. J. Control Release. 63: 235-259.   DOI
12 Solanki, N. D., S. Shah, J. Patel, and P. Upadhyay (2013) Formulation and evaluation of once a day bilayer floating tablet of antihypertensive drug involving dissolution enhancement approach. Der Pharmacia Sinica. 4: 54-66.
13 Saito, N., K. Konishi, F. Sato, M. Kato, H. Takeda, T. Sugiyama, and M. Asaka (2003) Plural transformation-processes from spiral to coccoid Helicobacter pylori and its viability. J. Infect. 46: 49-55.   DOI
14 Park, K. N. and J. R. Robinson (1984) Bioadhesive polymers as platforms for oral-controlled drug delivery: method to study bioadhesion. Int. J. Pharm. 19: 107-127.   DOI
15 Cockburn, J., A. L. Reid, J. A. Bowman, and R. W. Sanson-Fisher (1987) Effects of intervention on antibiotic compliance in patients in general practice. Med. J. Aust. 147: 324-328.
16 Chitnis, V. S., V. S. Malshe, and J. K. Lalla (1991) Bioadhesive polymers-synthesis, evaluation and application in controlled release tablets. Drug Dev. Ind. Pharm. 17: 879-892.   DOI
17 Hingmire, L. P. and D. M. Sakarkar (2013) Formulation and evaluation of Valsartan SR tablets using hydrophilic and hydrophobic polymer. J. Chem. Pharm. Sci. 6: 254-260.
18 Ha, N. S., T. T. Tran, P. H. Tran, J. B. Park, and B. J. Lee (2011) Dissolution-enhancing mechanism of alkalizers in poloxamer-based solid dispersions and physical mixtures containing poorly watersoluble valsartan. Chem. Pharm. Bull. 59: 844-880.   DOI
19 Xu, W. J., Y. Liu, L. L. Shi, J. H. Cui, and Q. R. Cao (2014) In vitro dissolution and physicochemical characterizations of novel PVPbased solid dispersion containing valsartan prepared by a freezedrying method. J. Pharm. Sci. 27: 1799-1804.
20 Serajuddin, A. T. M. (1999) Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs. J. Pharm. Sci. 88: 1058-1066.   DOI
21 Siepmann, J. and N. A. Peppas (2001) Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv. Drug Deliv. Rev. 48: 139-157.   DOI
22 US Pharmacopoeia National Formulary (2003) USP 26-NF21. 3rd ed., pp. 2439. Mack Printing Company, Easton, USA.
23 Ministry of Food and Drug Safety, Guideline on validation of analytical procedure. http://www.mfds.go.kr. (2015).
24 Talegaonikar, S., A. Y. Khan, R. K. Khar, F. J. Ahmad, and Z. Khan (2007) Development and characterization of Paracetamol complexes with hydroxypropyl ${\beta}$-cyclodextrin. Iranian J. Pharm. Res. 6: 95-99.
25 Baboota, S., M. Dhaliwal, and K. Kohli (2005) Physicochemical characterization, in vitro dissolution behavior, and pharmacodynamic studies of Rofecoxib-cyclodextrin inclusion compounds. Preparation and properties of Rofecoxib hydroxypropyl ${\beta}$-cyclodextrin inclusion complex: A technical note. AAPS Pharm. Sci. Tech. 6: 83-90.   DOI
26 Fouladi, F. and S. A. Mortazavi (2012) Preparation and in vitro evaluation of gastroretensive Bupropion hydrochloride tablets. Trop. J. Pharm. Res. 11: 351-359.
27 Ritger, P. L. and N. A. Peppas (1987) A simple equation for description of solute release II. Fickian and anomalous release from swellable devices. J. Controll. Rel. 5: 37-42.   DOI
28 Chen, R. N., H. O. Ho, C. Y. Yu., and M. T. Sheu (2010) Development of swelling / floating gastroretensive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose for Losartan and its clinical relevance in healthy volunteers with CYP2C9 polymorphism. Eur. J. Pharm. Sci. 39: 82-89.   DOI